For research use only. Not for therapeutic Use.
(D)-PPA 1 TFA is a hydrolysisresistant d-peptide antagonist. (D)-PPA 1 TFA serves as a potent PD-1/PD-L1 inhibitor. (D)-PPA 1 TFA binds to PD-1 with the affinity 0f 0.51 μM with in vitro and in vivo efficacy[1].
(D)-PPA 1 TFA (0.2 mg/mL, 1.0 mg/mL) blocks the interaction between PD-1/PD-L1 at 1.0 mg/mL[1].
(D)-PPA 1 TFA (3.125-100 μM; 24 h, 48 h) doesn’t kill tumor cells directly with no affect on CT26 cells growth[1].
(D)-PPA 1 TFA (2 mg/kg; s.c. or i.p.; once daily for 7 d) inhibits CT26 tumor growth in vivo in mice[1].
(D)-PPA 1 TFA (40 μg/mouse in 200 μL; i.v.; single dose) has the ability to target to tumor tissue in CT26-tumor-bearing mice[1].
| Catalog Number | I041207 |
| Synonyms | (3S)-4-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(1S)-1-carboxy-2-phenylethyl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-[[(2S,3R)-2-[[(2S)-1-[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2,4-diamino-4-oxobutanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]pyrrolidine-2-carbonyl]amino]-3-hydroxybutanoyl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic acid |
| Molecular Formula | C72H99F3N20O23 |
| Purity | ≥95% |
| InChI | InChI=1S/C70H98N20O21.C2HF3O2/c1-36(92)57(89-66(107)53-13-8-26-90(53)68(109)46(11-5-6-24-71)82-65(106)52(34-91)88-62(103)47(27-38-14-18-41(93)19-15-38)83-58(99)43(72)31-55(74)96)67(108)86-50(32-56(97)98)64(105)80-44(12-7-25-78-70(75)76)59(100)81-45(22-23-54(73)95)60(101)84-48(28-39-16-20-42(94)21-17-39)61(102)85-49(30-40-33-77-35-79-40)63(104)87-51(69(110)111)29-37-9-3-2-4-10-37;3-2(4,5)1(6)7/h2-4,9-10,14-21,33,35-36,43-53,57,91-94H,5-8,11-13,22-32,34,71-72H2,1H3,(H2,73,95)(H2,74,96)(H,77,79)(H,80,105)(H,81,100)(H,82,106)(H,83,99)(H,84,101)(H,85,102)(H,86,108)(H,87,104)(H,88,103)(H,89,107)(H,97,98)(H,110,111)(H4,75,76,78);(H,6,7)/t36-,43+,44+,45+,46+,47+,48+,49+,50+,51+,52+,53+,57+;/m1./s1 |
| InChIKey | WFYLZRHZVBLQEG-KCTFYJEASA-N |
| SMILES | CC(C(C(=O)NC(CC(=O)O)C(=O)NC(CCCNC(=N)N)C(=O)NC(CCC(=O)N)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)NC(CC2=CNC=N2)C(=O)NC(CC3=CC=CC=C3)C(=O)O)NC(=O)C4CCCN4C(=O)C(CCCCN)NC(=O)C(CO)NC(=O)C(CC5=CC=C(C=C5)O)NC(=O)C(CC(=O)N)N)O.C(=O)(C(F)(F)F)O |
| Reference | [1]. Chang HN, et al. Blocking of the PD-1/PD-L1 Interaction by a D-Peptide Antagonist for Cancer Immunotherapy. Angew Chem Int Ed Engl. 2015 Sep 28;54(40):11760-4. |
